PMID- 30301369
OWN - NLM
STAT- MEDLINE
DCOM- 20200728
LR  - 20200728
IS  - 1029-2330 (Electronic)
IS  - 1026-7158 (Linking)
VI  - 27
IP  - 4
DP  - 2019 Apr
TI  - GZD2202, a novel TrkB inhibitor, suppresses BDNF-mediated proliferation and 
      metastasis in neuroblastoma models.
PG  - 442-450
LID - 10.1080/1061186X.2018.1533964 [doi]
AB  - Collective data suggest tropomyosin-related kinase B (TrkB), which is correlated 
      with the growth, migration and poor prognosis of neuroblastoma (NB), is a 
      potential target for NB target therapy. Several Phase I/II pan-Trk inhibitors 
      display impressive clinical outcomes but still no drug has been approved for 
      general use. In this paper, we report a novel structural TrkB inhibitor GZD2202, 
      a structural derivative of our previously identified DDR1 antagonists. GZD2202 
      demonstrates a moderate selectivity between Trk B/C and TrkA. GZD2202 suppresses 
      the brain-derived neurotrophic factor (BDNF) -mediated TrkB signalling pathway, 
      proliferation, migration and invasion in SH-SY5Y-TrkB neuroblastoma cells, and 
      causes about 36.1% growth inhibition in a SH-SY5Y-TrkB neuroblastoma xenograft 
      model.
FAU - Zou, Jian
AU  - Zou J
AD  - a School of Pharmacy , Jinan University , Guangzhou , China.
FAU - Zhang, Zhang
AU  - Zhang Z
AD  - b International Cooperative Laboratory of Traditional Chinese Medicine 
      Modernization and Innovative Drug Development of Chinese Ministry of Education 
      (MOE), School of Pharmacy , Jinan University , Guangzhou , China.
AD  - c Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of 
      Pharmacy , Jinan University , Guangzhou , China.
FAU - Xu, Fang
AU  - Xu F
AD  - b International Cooperative Laboratory of Traditional Chinese Medicine 
      Modernization and Innovative Drug Development of Chinese Ministry of Education 
      (MOE), School of Pharmacy , Jinan University , Guangzhou , China.
AD  - c Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of 
      Pharmacy , Jinan University , Guangzhou , China.
FAU - Cui, Shengyang
AU  - Cui S
AD  - d University of Chinese Academy of Sciences , Beijing , China.
AD  - e Guangzhou Institutes of Biomedicine and Health , Chinese Academy of Sciences , 
      Guangzhou , China.
FAU - Qi, Chunli
AU  - Qi C
AD  - f Insititute of Laboratory Animal Science , Jinan University , Guangzhou , China.
FAU - Luo, Jinfeng
AU  - Luo J
AD  - e Guangzhou Institutes of Biomedicine and Health , Chinese Academy of Sciences , 
      Guangzhou , China.
FAU - Wang, Zhen
AU  - Wang Z
AD  - d University of Chinese Academy of Sciences , Beijing , China.
AD  - e Guangzhou Institutes of Biomedicine and Health , Chinese Academy of Sciences , 
      Guangzhou , China.
FAU - Lu, Xiaoyun
AU  - Lu X
AD  - b International Cooperative Laboratory of Traditional Chinese Medicine 
      Modernization and Innovative Drug Development of Chinese Ministry of Education 
      (MOE), School of Pharmacy , Jinan University , Guangzhou , China.
AD  - c Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of 
      Pharmacy , Jinan University , Guangzhou , China.
FAU - Tu, Zhengchao
AU  - Tu Z
AD  - a School of Pharmacy , Jinan University , Guangzhou , China.
AD  - e Guangzhou Institutes of Biomedicine and Health , Chinese Academy of Sciences , 
      Guangzhou , China.
FAU - Ren, Xiaomei
AU  - Ren X
AD  - b International Cooperative Laboratory of Traditional Chinese Medicine 
      Modernization and Innovative Drug Development of Chinese Ministry of Education 
      (MOE), School of Pharmacy , Jinan University , Guangzhou , China.
AD  - c Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of 
      Pharmacy , Jinan University , Guangzhou , China.
FAU - Song, Liyan
AU  - Song L
AD  - a School of Pharmacy , Jinan University , Guangzhou , China.
FAU - Ding, Ke
AU  - Ding K
AUID- ORCID: 0000-0001-9016-812X
AD  - b International Cooperative Laboratory of Traditional Chinese Medicine 
      Modernization and Innovative Drug Development of Chinese Ministry of Education 
      (MOE), School of Pharmacy , Jinan University , Guangzhou , China.
AD  - c Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of 
      Pharmacy , Jinan University , Guangzhou , China.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20181030
PL  - England
TA  - J Drug Target
JT  - Journal of drug targeting
JID - 9312476
RN  - 0 (Brain-Derived Neurotrophic Factor)
RN  - 0 (Protein Kinase Inhibitors)
RN  - 7171WSG8A2 (BDNF protein, human)
RN  - EC 2.7.10.1 (Receptor, trkB)
SB  - IM
MH  - Animals
MH  - Brain-Derived Neurotrophic Factor/metabolism
MH  - Cell Line, Tumor
MH  - Cell Movement/drug effects
MH  - Cell Proliferation/drug effects
MH  - Humans
MH  - Male
MH  - Mice
MH  - Mice, SCID
MH  - Neoplasm Invasiveness
MH  - Neoplasm Metastasis
MH  - Neuroblastoma/*drug therapy/pathology
MH  - Protein Kinase Inhibitors/*pharmacology
MH  - Receptor, trkB/*antagonists & inhibitors
MH  - Signal Transduction/drug effects
MH  - Xenograft Model Antitumor Assays
OTO - NOTNLM
OT  - BDNF
OT  - GZD2202
OT  - Tropomyosin receptor kinase B
OT  - neuroblastoma
EDAT- 2018/10/12 06:00
MHDA- 2020/07/29 06:00
CRDT- 2018/10/11 06:00
PHST- 2018/10/12 06:00 [pubmed]
PHST- 2020/07/29 06:00 [medline]
PHST- 2018/10/11 06:00 [entrez]
AID - 10.1080/1061186X.2018.1533964 [doi]
PST - ppublish
SO  - J Drug Target. 2019 Apr;27(4):442-450. doi: 10.1080/1061186X.2018.1533964. Epub 
      2018 Oct 30.